现货，WZ4002，selleck，美国进口，EGFR YZ剂，CAS号: 1213269-23-8 ，目录号 S1173_详细资料

产品信息

保质期：两年数量：大量英文名： WZ4002 CAS号： 1213269-23-8 供应商： selleck中国广州办事处保存条件：零下20摄氏度低温保存规格： 50片/10mg

规格： 50片产品价格：￥2268

规格： 10mg 产品价格：￥2268

S1173 WZ4002
信号转导通路: 受体酪氨酸激酶(RTK) >> EGFR >> EGFR YZ剂 >> WZ4002
技术数据:

分子量(MW): 494.18

化学式:
C₂₅H₂₇ClN₆O₃

溶解度: DMSO ≥13mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 1213269-23-8

生物活性

WZ4002不可逆YZ表皮生长因子T790M突变，IC50<20nM。WZ4002不可逆YZ表皮生长因子T790M突变,这种突变是在50%抗gefitinib和 erlotinib的患者身上发现的。WZ4002
有着和其他EGFRYZ剂不同的基本化学结构。与体内带有喹唑啉基的EGFRYZ剂HKI-272 和CL-387,785相比，WZ4002作用于EGFR T790M突变型时效果强30-100倍，而作用于野生型EGFR时效果弱到100倍。低于YZ浓度的一半的WZ4002和其他还处于临床阶段的YZ剂如HKI-272联用作用于PC9GR(delE746_A750/T790M,抗gefitinib的突变) 细胞，效果达到300倍。在两周的有效研究中发现，同时作用于鼠类T790M突变，与空白对照组相比，用WZ4002处理导致肿瘤的明显退化。WZ4002目前还处在临床研究阶段。WZ4002Z初是由波士顿的Dana Farber癌症研究所研究的。^[1]

参考文献

[1] Nature. 2009 December 24; 462(7276): 1070–1074.
[2] Cancer Cell.2007 Mar;11(3):217-27
[3] Science.2007 May 18;316(5827):1039-43. Epub 2007 Apr 26

客户反馈数据

(a) Western blots examine the effects of WZ4002 alone or a combination of WZ4002 and ABT-263 in H1975 parental or SR cells in suspension. Cells were grown for 48 h and then treated with the indicated pharmacological agent(s) for another 24 h. The cleaved/total poly (ADP-ribose) polymerase-1 (PARP-1) ratio determined for each cell line using Image J software is also represented. The values are the means of three independent experiments. (b) Quantification of apoptotic cells assessed by PARP-1 cleavage from each cell line.

Caspase 3/7 activation in H1975 SR cells and HCC827 cells. Cells were seeded and left in suspension for 24 h, and then untreated or treated with the indicated drug(s) for another 24 h before being assessed. Caspase activity was evaluated by using the Caspase-Glo 3/7 assay and normalized to a 1.0 arbitrary unit for the mean of three untreated wells.

For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ4002 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

如果需要长期保存，请于零下二十度低温保存。

禁止用于人体及ZL！

特定的存储和包装每个产品的信息在产品说明书上都有注明。大多数Selleck产品，在推荐的条件下存储可稳定保存两年。产品有时建议的储存温度不同，大多数建议储存在-20 ° C ，抗体及蛋白等产品建议-60℃。YZ剂属于化学试剂，可在常温下运输储存两周左右。即使如此，我们保证产品的出货量将保持产品质量的条件下，一般都会放入冰袋。望阁下收到产品后，请按照产品数据表建议适当存储。

温馨提示：不可用于临床ZL。

规格：	50片	产品价格：	￥2268
规格：	10mg	产品价格：	￥2268

分子量(MW):	494.18
化学式:	C₂₅H₂₇ClN₆O₃
溶解度:	DMSO ≥13mg/mL Water <1mg/mL Ethanol <1mg/mL
纯度:	>99%
稳定性:	at -20℃ 2 years
CAS号:	1213269-23-8

	(a) Western blots examine the effects of WZ4002 alone or a combination of WZ4002 and ABT-263 in H1975 parental or SR cells in suspension. Cells were grown for 48 h and then treated with the indicated pharmacological agent(s) for another 24 h. The cleaved/total poly (ADP-ribose) polymerase-1 (PARP-1) ratio determined for each cell line using Image J software is also represented. The values are the means of three independent experiments. (b) Quantification of apoptotic cells assessed by PARP-1 cleavage from each cell line.
	Caspase 3/7 activation in H1975 SR cells and HCC827 cells. Cells were seeded and left in suspension for 24 h, and then untreated or treated with the indicated drug(s) for another 24 h before being assessed. Caspase activity was evaluated by using the Caspase-Glo 3/7 assay and normalized to a 1.0 arbitrary unit for the mean of three untreated wells.
	For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of WZ4002 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 mM HCl and 0.1% Nonidet-40) was added to dissolve the formazan.

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现货，WZ4002，selleck，美国进口，EGFR YZ剂 ，CAS号: 1213269-23-8 ，目录号 S1173

产品信息

现货，WZ4002，selleck，美国进口，EGFR YZ剂，CAS号: 1213269-23-8 ，目录号 S1173